2. GPCR/G Protein NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Angiotensin Receptor Reactive Oxygen Species Apoptosis
  4. Azilsartan

Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research.

For research use only. We do not sell to patients.

Azilsartan Chemical Structure

Azilsartan Chemical Structure

CAS No. : 147403-03-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 44 In-stock
Solution
10 mM * 1 mL in DMSO USD 44 In-stock
Solid
25 mg USD 40 In-stock
50 mg USD 60 In-stock
100 mg USD 100 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Azilsartan:

Azilsartan Related Antibodies

Top Publications Citing Use of Products

    Azilsartan purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Apr 11;8(15):24099-24109.  [Abstract]

    Rats are orally administered with vehicle or Azilsartan (5 mg/kg/d) during the four-week rotenone (2.5 mg/kg/d) infusion. A. TH-immunoreactive neurons in the SN of each group. B. Quantitative analysis of TH-positive neurons in the SN of each group. Scale bar: 500 μm. C. The activity of caspase-3 in the SN is measured by a colorimetric assay kit.

    View All Angiotensin Receptor Isoform Specific Products:

    View All Isoforms
    AT1 Receptor AT2 Receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[1][2][3][4][5].

    IC50 & Target

    AT1 Receptor

     

    In Vitro

    Azilsartan (0-200 μM, 0-72 h) decreases the viability of HepG2 cells[5].
    Azilsartan (100 μM, 24 h) induces apoptosis in HepG2 cells[5].
    Azilsartan inhibits the specific binding of 125I-Sar1-Ile8-AII to human angiotensin type 1 receptors with an IC50 of 2.6 nM[3].
    Azilsartan potently inhibits aortic endothelial and vascular cell proliferation in the absence of exogenous Ang II supplementation[5].
    Azilsartan enhances adipogenesis and exerted greater effects than Valsartan (HY-18204) on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Azilsartan Related Antibodies

    Cell Proliferation Assay[5]

    Cell Line: HepG2 and KDR cells
    Concentration: 5, 25, 50, 100 and 200 μM
    Incubation Time: 24, 48, and 72 h
    Result: Gradually decreased the viability of HepG2 cells by increasing the incubation time and dose, the inhibitory concentration of Azilsartan (IC 50%) against HepG2 cells was 100 μM for 24 h treatment time point while in KDR epithelial normal cells no significant cytotoxic effect was observed during the similar treatment conditions.

    Apoptosis Analysis[5]

    Cell Line: HepG2 cells
    Concentration: 100 μM
    Incubation Time: 24 h
    Result: Induced 57.2% early and 0.52% late apoptosis respectively after 24 h.
    In Vivo

    Azilsartan (0-3 mg/kg, Oral gavage, once daily for 5 days) decreases SBP (systolic blood pressure) in obese Koletsky rats at 2 mg/kg[2].
    Azilsartan (0-2 mg/kg, Oral gavage, once daily for 21 days) lowers blood pressure and basal plasma insulin concentration[2].
    Azilsartan (2 and 4 mg/kg; PO, daily for 9 days) offers protection against ischemia induced secondary brain injury[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male Wistar-Kyoto (WKY) rats, obese Koletsky rats (n=6 per group)[2]
    Dosage: 0, 1, 2 and 3 mg/kg
    Administration: Oral gavage, once daily (9:00-10:00 hours) for 5 days
    Result: Decreased SBP (systolic blood pressure) in obese Koletsky rats to that of normal rats at 2 mg/kg, whereas the 3 mg/kg dose elicited hypotension.
    Animal Model: Obese Koletsky rats (16, n = 8 per group)[2]
    Dosage: 0 and 2 mg/kg
    Administration: Oral gavage, once daily (9:00-10:00 hours) for 21 days
    Result: Lowered blood pressure, basal plasma insulin concentration and the homeostasis model assessment of insulin resistance index, and inhibited over-increase of plasma glucose and insulin concentrations during oral glucose tolerance test.
    Animal Model: Male Wistar Rats (240–280 g)[4]
    Dosage: 0, 2, and 4 mg/kg
    Administration: Orally, daily for 9 days, starting 7 days before the day of surgery
    Result: Individual treatments with Azilsartan (2 & 4 mg/kg) and Coenzyme Q10 (HY-N0111) (20 & 40 mg/kg) significantly attenuated the reduction in locomotor activity. Further, combination treatment with azilsartan (2 mg/kg) and Coenzyme Q10 (20 mg/kg) significantly improved the locomotor activity of animals as compared to their effects per se in BCCAO treated animals.
    Clinical Trial
    Molecular Weight

    456.45

    Formula

    C25H20N4O5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C2C(N=C(OCC)N2CC3=CC=C(C4=CC=CC=C4C(N5)=NOC5=O)C=C3)=CC=C1)O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (54.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1908 mL 10.9541 mL 21.9082 mL
    5 mM 0.4382 mL 2.1908 mL 4.3816 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1908 mL 10.9541 mL 21.9082 mL 54.7705 mL
    5 mM 0.4382 mL 2.1908 mL 4.3816 mL 10.9541 mL
    10 mM 0.2191 mL 1.0954 mL 2.1908 mL 5.4771 mL
    15 mM 0.1461 mL 0.7303 mL 1.4605 mL 3.6514 mL
    20 mM 0.1095 mL 0.5477 mL 1.0954 mL 2.7385 mL
    25 mM 0.0876 mL 0.4382 mL 0.8763 mL 2.1908 mL
    30 mM 0.0730 mL 0.3651 mL 0.7303 mL 1.8257 mL
    40 mM 0.0548 mL 0.2739 mL 0.5477 mL 1.3693 mL
    50 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0954 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Azilsartan Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Azilsartan147403-03-0TAK-536TAK536TAK 536Angiotensin ReceptorReactive Oxygen SpeciesApoptosisHypertensionNeuroprotectionStrokeIschemiaHepG2KDR cellsendothelialvascular cellcanceradipogenesisInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Azilsartan
    Cat. No.:
    HY-14914
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (392 KB) Français - FR (392 KB) Deutsch - DE (392 KB) Norwegian - NO (392 KB) Español - ES (392 KB) Swedish - SV (392 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.